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CompletedNCT03441841Updated Feb 22, 2018

Pharmacokinetic Study of Nanoencapsulated Gel of Lidocaine, Prilocaine and Combination of Lidocaine and Prilocaine

A Phase 1 interventional study of Lidocaine + Prilocaine and Lidocaine in Topical Anesthesia, sponsored by Galeno Desenvolvimento de Pesquisas Clínicas. Completed at 1 site in Brazil. Open to participants aged 19 Years to 53 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2018-02-22.

Sponsored by Galeno Desenvolvimento de Pesquisas Clínicas · Phase 1, Interventional, and Treatment

Phase
Phase 1
Study type
Interventional
Enrollment
48
Allocation
Randomized
Ages
19 Years to 53 Years
Sex
All
01

Study summary

This trial evaluated the pharmacokinetic interaction between fixed doses of lidocaine (2.5%), prilocaine (2.5%) or the association of both (Nanorap®) in healthy volunteers. The drug safety and tolerability was also evaluated.

Read the detailed description

This study was performed as a monocentric, open, randomized, double-blind, with 3 treatment regimen (lidocaine, prilocaine, or Nanorap®) in 3 periods design. Volunteers were submitted to clinical and laboratory examination before enrollment. Treatments were carried out on 3 different days with a washout period of 7 days between each dose.

After a fasting period (8 h), volunteers received topically 2g of the formulation in a delimited area of 16 cm2 in the volar surface of the forearm. The product was applied to the left arm and venous blood was collected from the right arm. The remaining product was removed with a cotton swab 10 minutes after application. Blood samples (3.5 mL) were collected into heparinized tubes before (0:00) and at 1.0, 2.0, 3.0, 4.0, 4.5, 5.0, 5.5, 6.0, 6.5, 7.0, 7.5, 8.0, 8.5, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0 and 24.0 h after the hydrogel application.

Blood samples were centrifuged at 2000 g (4 ⁰C) for 10 minutes and the obtained plasma samples were stored at -20 °C until analysis.

Following dosing, volunteers were monitored for 36 h in a clinical setting safety and tolerability (signs, symptoms, adverse events, and laboratory parameters). The vital signs (blood pressure and pulse rate) were evaluated. ECGs were obtained before (30 min) and at drug Cmax (6 h) for each product application. QT interval corrected by heart rate (QTc) data were obtained from a Bionet Cardiocare 2000 and BMS-Plus software program, using Bazett's formula: QTc = QT/(sqrt RR Interval).

02

Conditions studied

  • Topical Anesthesia

Keywords

  • local anesthetics
  • pharmacokinetics
  • nanotechnology
03

Who can participate

Ages eligible
19 Years to 53 Years
Sexes eligible
All
Accepts healthy volunteers
Yes

Inclusion criteria

  • Healthy volunteers over 18 years old
  • Body mass index (BMI) ≥ 19.0 kg/m² and ≤ 28.75 kg/m²
  • No evidence of significant diseases, that, at the investigator's discretion, may affect the participation in the clinical trial, in accordance with the protocol requirements
  • Ability to understand the nature and the objective of the clinical trial,including the risks and possible side effects; intention to cooperate with the investigator and act in accordance with the protocol requirements, as confirmed by the informed consent form signature.

Exclusion criteria

Exclusion Criteria:

  • Subjects with known hypersensitivity to the compounds of the investigational products, severe allergies or multiple drug allergies
  • Existing diseases or pathological findings, which might interfere with the safety or tolerability, and/or pharmacokinetics of the drug
  • Screening laboratory tests presenting deviations deemed as clinically significant, which, due to possible risks, prevents the participation in clinical trial.
  • Use of maintenance therapy with any drug
  • Drug or alcohol dependence
  • Volunteers who ingests more than 5 cups of coffee or tea per day and/or smoke
  • Volunteers with unusual eating habits, e.g, vegetarian
  • Treatment, within 3 months prior to the initiation of the clinical trial treatment, with any drug known to have a well-established toxic potential to major organs.
  • Use of regular medication within 2 weeks before the start of treatment and the date of evaluation, or made use of any medication within one week, except for oral contraceptives or cases where, based on the half-life of the drug and/or active metabolites, complete elimination can be assumed
  • Treatment within 6 months prior to the study with any known drug of have a well-defined toxic potential in large organs
  • Hospitalization for any reason up to 8 weeks before the start of the treatment of this study
  • Participation in a clinical trial during the last 6 months
  • Blood donation or other blood loss of more than 450 mL within the last 3 months
  • Pregnant, delivery or abortion in the 12 weeks prior to the planned hospitalization
  • The volunteer who has any condition that prevents him from participating in the study by judgment of the investigator
04

Study design

Phase
Phase 1
Primary purpose
Treatment
Allocation
Randomized
Intervention model
Crossover assignment
Masking
None (open label)
Enrollment
48 participants (actual)

Study arms

  • Experimental
    Lidocaine + prilocaine

    Single topical dose of a combination of nanoencapsulated lidocaine (2.5%) and prilocaine (2.5%) formulation in a delimited area of 16 cm2 in the volar surface of the forearm.

    Drug: Lidocaine + Prilocaine

  • Active comparator
    Lidocaine

    Single topical dose of lidocaine nanoencapsulated gel (2.5 %) formulation in a delimited area of 16 cm2 in the volar surface of the forearm.

    Drug: Lidocaine

  • Active comparator
    Prilocaine

    Single topical dose of prilocaine (2.5 %) nanoencapsulated gel formulation in a delimited area of 16 cm2 in the volar surface of the forearm.

    Drug: Prilocaine

Interventions

  • DrugLidocaine + Prilocaine

    Single topical dose of 2g lidocaine + prilocaine 2.5 % formulation.

    Also known as: Nanorap®

  • DrugLidocaine

    Single topical dose of 2g lidocaine 2.5 % formulation.

  • DrugPrilocaine

    Single topical dose of 2g prilocaine 2.5 % formulation.

05

What researchers measure

Primary outcomes

  1. Measurement of lidocaine and prilocaine plasma levels

    Blood sampling for the determination of plasma levels of lidocaine and prilocaine in participants of each treatment group.

    Time frame: 0-24 h

  2. Maximum Plasma Concentration (Cmax) of lidocaine and prilocaine

    Determination of Cmax for lidocaine and prilocaine based on plasma concentrations of samples obtained.

    Time frame: 0-24 h

  3. Area Under the Curve (AUC) of lidocaine and prilocaine

    Determination of AUC for lidocaine and prilocaine based on plasma concentrations of samples obtained.

    Time frame: 0-24 h

Secondary outcomes

  1. Number of adverse events per participant

    Determination of the number of adverse events, in each treatment group, including clinically relevant alterations of vital signs and laboratory tests results.

    Time frame: Up to 36 h after treatment

06

Study locations

1 site
  • Galeno Desenvolvimento de Pesquisas Clinicas Ltda. - ME
    Campinas, SP, Brazil
07

References and documents

Individual participant data

Plan to share: No

No publications or documents are linked to this record.

08

Registry details

Key details

Study ID
NCT03441841
Lead sponsor
Galeno Desenvolvimento de Pesquisas Clínicas
Collaborators
Biolab Sanus Farmaceutica
Responsible party
Gilberto De Nucci (Doctor, Galeno Desenvolvimento de Pesquisas Clínicas) — Principal investigator
First posted
Feb 22, 2018
Start date
Feb 28, 2016
Primary completion
Mar 19, 2016
Completion
May 6, 2016
Last update
Feb 22, 2018

Oversight

Data monitoring committee
Yes
FDA-regulated drug
No
FDA-regulated device
No
View the source record on ClinicalTrials.gov ↗

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